Assay Detail
Binding
CHEMBL2330944
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Displacement of [125I]AB-MECA from human A3 adenosine receptor expressed in CHO cells after 60 mins by scintillation counting analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2-Arylpyrazolo[4,3-d]pyrimidin-7-amino derivatives as new potent and selective human A3 adenosine receptor antagonists. Molecular modeling studies and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 27 | 7.51 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2322924 | — | — | 1 | 8.62 |
| CHEMBL2322900 | — | — | 1 | 8.49 |
| CHEMBL2322927 | — | — | 1 | 8.28 |
| CHEMBL2322928 | — | — | 1 | 8.28 |
| CHEMBL2322923 | — | — | 1 | 8.25 |
| CHEMBL2322931 | — | — | 1 | 8.14 |
| CHEMBL582911 | — | — | 1 | 7.80 |
| CHEMBL2322898 | — | — | 1 | 7.75 |
| CHEMBL2322907 | — | — | 1 | 7.75 |
| CHEMBL2322930 | — | — | 1 | 7.70 |
| CHEMBL2322926 | — | — | 1 | 7.70 |
| CHEMBL2322899 | — | — | 1 | 7.62 |
| CHEMBL2322908 | — | — | 1 | 7.62 |
| CHEMBL2322901 | — | — | 1 | 7.60 |
| CHEMBL2322929 | — | — | 1 | 7.50 |
| CHEMBL2322910 | — | — | 1 | 7.48 |
| CHEMBL2322909 | — | — | 1 | 7.48 |
| CHEMBL2322903 | — | — | 1 | 7.46 |
| CHEMBL2322905 | — | — | 1 | 7.35 |
| CHEMBL2322920 | — | — | 1 | 7.12 |
| CHEMBL2322911 | — | — | 1 | 7.12 |
| CHEMBL2322906 | — | — | 1 | 7.01 |
| CHEMBL2322902 | — | — | 1 | 7.00 |
| CHEMBL2322925 | — | — | 1 | 6.92 |
| CHEMBL2322922 | — | — | 1 | 6.52 |
| CHEMBL2322904 | — | — | 1 | 6.28 |
| CHEMBL574417 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2322924 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL2322900 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL2322927 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL2322928 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL2322923 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL2322931 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL582911 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2322898 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2322907 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2322930 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2322926 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2322899 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2322908 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2322901 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2322929 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL2322910 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL2322909 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL2322903 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL2322905 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL2322920 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL2322911 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL2322906 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL2322902 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2322925 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2322922 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL2322904 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL574417 | — | Ki | = | 900.0 | nM | 6.05 |